ArticleMolecular diversity2026
Design, synthesis, and biological evaluation of novel isobenzofuran-1(3H)-one derivatives with antioxidant properties and improved oral bioavailability.
Article in Molecular diversity, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
Bioavailability is a critical determinant factor of a drug, especially for its therapeutic efficacy, safety and commercial feasibility. Many active small molecule drugs suffer from poor oral bioavailability. 3-Butylisobenzofuran-1(3H)-one (NBP) is an approved small molecule agent by the CFDA for the treatment of acute cerebral ischemic stroke. NBP inhibits platelet aggregation, reduces brain infarct size, and attenuates ischemic-induced oxidative damage. However, the efficacy of NBP is limited due to its low bioavailability and high hydrophobicity. Sometimes, administration of high doses and increased frequency of NBP causes hepatotoxicity. Here, we designed, synthesized and evaluated a series of novel 6-substituted 3-butylisobenzofuran-1(3H)-one derivatives in vitro and in vivo and compared them with NBP or Br-NBP. Several compounds in the series showed better protective effects by preventing H
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